132838-34-7

Upstream product

• 762-49-2 2-fluoroethyl bromide 
• 67-56-1 methanol 
• 702-18-1 1-Fluor-2-(p-methyl)phenoxyethan 
• 99-96-7 4-hydroxy-benzoic acid 
• 99-76-3 methyl 4-hydroxylbenzoate 

Downstream Products

• 373604-69-4 (4-(2-fluoroethoxy)phenyl)bis(4-methoxyphenyl)methanol 
• 145304-35-4 4-(2-fluoroethoxyl)benzoic acid 
• 1269797-25-2 4-(2-fluoroethoxy)-N-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)benzamide 
• 1269797-33-2 4-(2-fluoroethoxy)-N-(4-(4-(2-methoxyphenyl)piperazin-1-yl)-trans-butyl-2-enyl)benzamide 
• 1269797-49-0 4-(2-fluoroethoxy)-N-(4-(4-(2-(2-fluoroethoxy)phenyl)piperazin-1-yl)butyl)benzamide 
• 373604-71-8 1-{2-[[4-(2-fluoro-ethoxy)-phenyl]-bis-(4-methoxy-phenyl)-methoxy]-ethyl}-piperidine-3-carboxylic acid ethyl ester 
• 373604-70-7 C₂₃H₂₂ClFO₃ 
• 123644-45-1 1-(2-fluoroethoxy)-4-(bromomethyl)benzene 
• 93613-03-7 (4-(2-fluoroethoxy)phenyl)methanol 

Relevant academic research and scientific papers

Electro-Oxidative Selective Esterification of Methylarenes and Benzaldehydes

A mild and green electro-oxidative protocol to construct aromatic esters from methylarenes and alcohols is herein reported. Importantly, the reaction is free of metals, chemical oxidants, bases, acids, and operates at room temperature. Moreover, the design of the electrolyte was found critical for the oxidation state and structure of the coupling products, a rarely documented effect. This electro-oxidative coupling process also displays exceptional tolerance of many fragile easily oxidized functional groups such as hydroxy, aldehyde, olefin, alkyne, as well as neighboring benzylic positions. The enantiomeric enrichment of some chiral alcohols is moreover preserved during this electro-oxidative coupling reaction, making it overall a promising synthetic tool.

Design, Synthesis, and in Vitro and in Vivo Evaluation of an 18F-Labeled Sphingosine 1-Phosphate Receptor 1 (S1P1) PET Tracer

Sphingosine 1-phosphate receptor 1 (S1P1) plays a pivotal signaling role in inflammatory response; because S1P1 modulation has been identified as a therapeutic target for various diseases, a PET tracer for S1P1 would be a useful tool. Fourteen fluorine-containing analogues of S1P ligands were synthesized and their in vitro binding potency measured; four had high potency and selectivity for S1P1 (S1P1 IC50 100-fold selectivity for S1P1 over S1P2 and S1P3). The most potent ligand, 28c (IC50 = 2.63 nM for S1P1) was 18F-labeled and evaluated in a mouse model of LPS-induced acute liver injury to determine its S1P1-binding specificity. The results from biodistribution, autoradiography, and microPET imaging showed higher [18F]28c accumulation in the liver of LPS-treated mice than controls. Increased expression of S1P1 in the LPS model was confirmed by immunohistochemical analysis (IHC). These data suggest that [18F]28c is a S1P1 PET tracer with high potential for imaging S1P1 in vivo.

LABELED MOLECULAR IMAGING AGENTS AND METHODS OF USE

Imaging agents are described that comprise labeled substrates capable of being introduced into cells via the cystine/glutamate antiporter. The substrates may be used for imaging or detecting oxidative stress in cells by introducing the labeled agents into

Synthesis and pharmacological evaluation of fluorine-containing D 3 dopamine receptor ligands

A series of fluorine-containing N-(2-methoxyphenyl)piperazine and N-(2-fluoroethoxy)piperazine analogues were synthesized, and their affinities for human dopamine D2, D3, and D4 receptors were determined. Radioligand binding studies identified five compounds, 18a, 20a, 20c, 20e, and 21e, which bind with high affinity at D3 (K i = 0.17-5 nM) and moderate to high selectivity for D3 vs D2 receptors (ranging from ～25- to 163-fold). These compounds were also evaluated for intrinsic activity at D2 and D3 receptors using a forskolin-dependent adenylyl cyclase assay. This panel of compounds exhibits varying receptor subtype binding selectivity and intrinsic activity at D2 vs D3 receptors. These compounds may be useful for behavioral pharmacology studies on the role of D2-like dopamine receptors in neuropsychiatric and neurological disorders. Furthermore, compound 20e, which has the highest binding affinity and selectivity for the D3 receptor (Ki = 0.17 nM for D3, 163-fold selectivity for D3 vs D2 receptors), represents a candidate fluorine-18 radiotracer for in vivo PET imaging studies on the regulation of D3 receptor expression.

ISATIN ANALOGUES AND USES THEREFOR

Novel isatin analogues, including isatin analogues comprising Michael Acceptors (IMAs) are disclosed. Further disclosed are methods of synthesis of the isatin analogues, and uses of the analogues, including inhibition of caspase-3 and caspase-7, and in vi

Synthesis, radiolabeling, and in vivo evaluation of an 18F-labeled isatin analog for imaging caspase-3 activation in apoptosis

A non-peptide-based isatin sulfonamide analog, WC-II-89, was synthesized and its inhibition toward recombinant human caspase-3 and other caspases was determined. This compound showed high potency for inhibiting caspase-3 and -7, and high selectivity again

Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase

The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated β-amyloid deposits or β-amyloid levels in a patient.

Radiosynthesis of (±)-(2-((4-(2-[18F]fluoroethoxy)phenyl)bis(4-methoxy- phenyl) methoxy)ethylpiperidine-3-carboxylic acid: A potential GAT-3 PET ligand to study GABAergic neuro-transmission in vivo

A dysfunction of GABAergic neurotransmission is related to diseases such as epilepsy, Huntington-disease and Parkinson-syndrome. A new 18F-fluorine labelled GABA transporter ligand for the GABA-transporter subtype GAT-3 was developed which may allow the in vivo visualisation of GABAergic neurotransmission. The precursors ethyl (2-(4-hydroxyphenyl)bis (4-methoxyphenyl)-methoxy)ethyl)-piperidine-3-carboxylate and ethyl(2-((4-(2-tosylethoxy)phenyl)-bis(4-methoxyphenyl)-methoxy) ethyl)piperidine-3-carboxylate were synthesised and labelled by the use of 2-[18F]fluoroethyltosylate or [18F]fluoride. Subsequent cleavage of the ester moiety gave the final product (±)-(2-((4-(2-[18F]fluoroethoxy)phenyl)bis(4-methoxy- phenyl)methoxy)ethyl)-piperidine-3-carboxylic acid in a decay corrected yield of 33-36%. Preliminary biodistribution kinetics were determined with BALB/c mice ex vivo for brain, liver, kidney, spleen, blood and bone. (2-((4-(2-[18F]fluoroethoxy)-phenyl)bis(4-methoxyphenyl)methoxy)- ethyl) piperidine-3-carboxylic acid showed a maximum brain uptake after 1 h p.i. of about 0.3% ID/g. Copyright